Chalcone belongs to a genus of flavonoid compounds. In natural products, chalcone principally exists in plants such as Asteraceae, Lauraceae, Liliaceae and so on.
The basic structure of chalcone is shown as follows.

Chalcones and their derivatives have been found to have bactericidal, anti-fungal, anti-cancer, and anti-inflammatory activities and so on, and have sugariness and the characteristic of drug. For instance, para-hydroxy (2′-hydroxy or 6′-hydroxy) is the essential substituent for bactericidal activity, 2′,4′-dihydroxy 3,4-dihydroxy and 2′,4′-dihydroxy 4-hydroxy chalcone derivatives have inhibition activity of aldose reductase and thus can be drugs for reducing or delaying the complications of diabetes (Severi et al., Eur. J. Med. Chem. 1998, 33(11): 859-866); 2,4,5-methoxy 3′,6′-dihydroxy chalcone derivative isolated from Fissistigma lanuginosum can inhibit tubulins to polymerize as microtubules (Alias et al., J. Nat. Prod. 1995, 58(8): 1160-1166); and 2′,3,4-trihydroxy 5′-methyl, and 2′,3,4-trimethyl 5′-isopropyl chalcone derivatives have topical anti-inflammatory activity (Sogawa et al., J. Med. Chem. 1993, 36(24): 3904-3909).
The current hypoglycemic medicines include sulfonylurea insulin secretagogues, non-sulfonylurea insulin secretagogues, biguanides, α-glucosidase inhibitors (AGI), thiozidinediones (TZDs, or insulin sensitizers) and dipeptidyl peptidase IV inhibitors (DPP-4 inhibitor). However, they represent side effects with different severity levels. For instance, metformin, a species of biguanides, generates side effects of diarrhea, anorexia, vomit and the most seriously lethal lactic acidosis. Acarbose, a species of AGI, is capable of generating side effect on gastrointestinal tract.
Insulin sensitizers include troglitazone, rosiglitazone (RSZ), pioglitazone (PIO), etc. This types of medicines can enhance the sensitivity of peripheral tissues to insulin, cannot stimulate insulin secretion, intervene to regulate gene transcription of cells via peroxisome proliferator activated receptor gamma (PPARγ) to increase the synthesis of glucose transporter in cells and enhance the glucose usage in cells, and thus decrease the glucose level in the blood. However, the adverse drug reaction of this medicine includes edema, body weight gain, congestive heart failure and the severest hepatotoxicity. Therefore, searching novel anti-hyperglycemic agent without the aforementioned side effects becomes a new issue on new drug development.
It is therefore attempted by the applicant to deal with the above situation encountered in the prior art.